Analyzing the synthesis route of 4-(Difluoromethoxy)benzene-1,2-diamine

At the same time, in my other blogs, there are other synthetic methods of this type of compound, 4-(Difluoromethoxy)benzene-1,2-diamine, and friends who are interested can also refer to it.

Adding a certain compound to certain chemical reactions, such as: 172282-50-7, name is 4-(Difluoromethoxy)benzene-1,2-diamine, belongs to ethers-buliding-blocks compound, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 172282-50-7, SDS of cas: 172282-50-7

Preparation of Intermediate C7. Step 1 . Preparation of C7-1 : To a solution of C4-1 (1 .84 g, 10.93 mmol) and 4-(difluoromethoxy)benzene-1 ,2-diamine (1 .90 g, 10.93 mmol, prepared according to Reference Example 30y of International Patent Publication No. WO 2003/035065, p. 51 1 .) in DMF (40 mL) at rt was added DIPEA (9.5 mL, 54.65 mmol) and HATU (6.23 g, 16.4 mmol). The reaction mixture was stirred at room temperature for 24 h, diluted with ethyl acetate (100 mL), washed with water (100 mL) and brine (50 mL). The mixture was concentrated in vacuo. Purification via silica gel chromatography (EtOAc in hexanes: 20% to 60%) provided C7-1 as the later eluting fraction of two with the similar mass spectra. LCMS-ESr (m/z): [M+H]+ calcd for Ci2H9F4N2O: 289.2; found: 289.0.

At the same time, in my other blogs, there are other synthetic methods of this type of compound, 4-(Difluoromethoxy)benzene-1,2-diamine, and friends who are interested can also refer to it.

Reference:
Patent; GILEAD SCIENCES, INC.; BJORNSON, Kyla; KARKI, Kapil K.; LINK, John O.; PYUN, Hyung-Jung; SCHRIER, Adam J.; STEVENS, Kirk L.; TAYLOR, James G.; VIVIAN, Randall W.; ZABLOCKI, Jeff; ZIPFEL, Sheila; WO2014/145095; (2014); A1;,
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